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Bupropion

bupropion

Basic Information

Summary

A frequently prescribed atypical antidepressant. Occasionally prescribed as an aid to smoking cessation. May lower seizure threshold in predisposed individuals. Poorly understood mechanism of action, probably an NDRI. Avoid combination with other drugs.

Stimulant

Stimulants excite the nervous system and increase physiological function.

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Habit-forming

These drugs pose a higher risk of causing habit forming behaviour, take particular care with the amount and frequency they are taken.

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Duration

Parent
Onset15-90 minutes
Duration11-21 hours
After-effects1-6 hours
Metabolites
Onset15-90 minutes
Duration20-37 hours
After-effects1-6 hours

General-effects

Mild - moderate increase in motor activity and agitation/excitement

Adverse-effects

Agitation, dry mouth, insomnia, headache/migraine, nausea/vomiting, constipation, tremor, dizziness, excessive sweating, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmia, and auditory disturbance

Overdose-symptoms

Seizure, hallucinations, loss of consciousness, sinus tachycardia, ECG changes, bradycardia, cardiac failure, cardiac arrest, and death

Warning

Bupropion lowers the seizure threshold and can induce seizures when excessive doses are used and/or when combined with CNS stimulants or other drugs that also lower the threshold, such as theophylline, steroids, some tricyclic antidepressants, and alcohol

Chemistry

IUPAC: (±)-2-(tert-Butylamino)-1-(3-chlorophenyl)propan-1-one | Formula: C13H18ClNO | Molecular Mass: 239.74 g/mol

Pharmacology

NDRI (Norepinephrine-Dopamine Reuptake Inhibitor); NDRA (Norepinephrine-Dopamine Releasing Agent); α3β2, α3β4, α4β2, and α7 nACh receptor antagonist

Pharmacokinetics

Protein Binding: 84% (bupropion), 77% [hydroxybupropion (active metabolite)], 42% [threohydrobupropion (active metabolite)] | Metabolism: hepatic, primarily CYP2B6-mediated hydroxylation; both bupropion and hydroxybupropion (active metabolite) are CYP2D6 inhibitors | Excretion: renal (87%; 0.5% unchanged) and faecal (10%)

Legal

Australia: Prescription Only (S4) | Canada: ℞-only | United Kingdom: POM | United States: ℞-only

Aliases

wellbutrin
zyban
amfebutamone

Contradictions

Seizure disorder, current or prior diagnosis of bulimia or anorexia nervosa, abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and anti-epileptic drugs, and MAOIs,

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Interactions

No interaction information for Bupropion

References & Notes

General